BR0015120A - Benzamidine derivative or a pharmaceutically acceptable salt thereof, pharmaceutical composition, and, use of a benzamidine derivative or a pharmaceutically acceptable salt thereof - Google Patents
Benzamidine derivative or a pharmaceutically acceptable salt thereof, pharmaceutical composition, and, use of a benzamidine derivative or a pharmaceutically acceptable salt thereofInfo
- Publication number
- BR0015120A BR0015120A BR0015120-3A BR0015120A BR0015120A BR 0015120 A BR0015120 A BR 0015120A BR 0015120 A BR0015120 A BR 0015120A BR 0015120 A BR0015120 A BR 0015120A
- Authority
- BR
- Brazil
- Prior art keywords
- group
- pharmaceutically acceptable
- optionally substituted
- benzamidine derivative
- acceptable salt
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 5
- 150000003937 benzamidines Chemical class 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- PXXJHWLDUBFPOL-UHFFFAOYSA-N benzamidine Chemical class NC(=N)C1=CC=CC=C1 PXXJHWLDUBFPOL-UHFFFAOYSA-N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 206010053567 Coagulopathies Diseases 0.000 abstract 1
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- -1 atom halogen Chemical class 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008177 pharmaceutical agent Substances 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Manufacture Of Alloys Or Alloy Compounds (AREA)
Abstract
"DERIVADO DE BENZAMIDINA OU UM SAL DESTE FARMACEUTICAMENTE ACEITáVEL, COMPOSIçãO FARMACêUTICA, AGENTE, E, USO DE UM DERIVADO DE BENZAMIDINA OU DE UM SAL DESTE FARMACEUTICAMENTE ACEITáVEL". Os derivados de benzamidina de fórmula (1) ou seus sais farmaceuticamente aceitáveis exibem excelente atividade inibidora contra o fator Xa e são úteis para tratar ou prevenir os distúrbios de coagulação do sangue: em que R^ 1^ representa um átomo de hidrogênio, um átomo de halogênio, um grupo alquila ou um grupo hidroxila; R^ 2^ representa um átomo de hidrogênio, um átomo de halogênio ou um grupo alquila, R^ 3^ representa um átomo de hidrogênio, um grupo alquila opcionalmente substituído, um grupo aralquila, um grupo alcanoíla opcionalmente substituído ou um grupo alquilsulfonila opcionalmente substituído, R^ 4^ e R^ 5^ são os mesmos ou diferentes um do outro e cada um representa um átomo de hidrogênio, um átomo de halogênio, um grupo alquila opcionalmente substituído, um grupo alcóxi, um grupo carboxila, um grupo alcoxicarbonila ou um grupo carbamoíla opcionalmente substituído e R^ 6^ representa um grupo pirrolidina substituído ou grupo piperidina substituído."BENZAMIDINE DERIVATIVE OR A SALT FROM THIS PHARMACEUTICALLY ACCEPTABLE, PHARMACEUTICAL COMPOSITION, AGENT, AND USE OF A BENZAMIDINE DERIVATIVE OR A PHARMACEUTICALLY ACCEPTED SALT". The benzamidine derivatives of formula (1) or their pharmaceutically acceptable salts exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood clotting disorders: where R ^ 1 ^ represents a hydrogen atom, an atom halogen, an alkyl group or a hydroxyl group; R ^ 2 ^ represents a hydrogen atom, a halogen atom or an alkyl group, R ^ 3 ^ represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group , R ^ 4 ^ and R ^ 5 ^ are the same or different from each other and each represents a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group and R6 is a substituted pyrrolidine group or substituted piperidine group.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP30719299 | 1999-10-28 | ||
| PCT/JP2000/007469 WO2001030756A1 (en) | 1999-10-28 | 2000-10-25 | Benzamidine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0015120A true BR0015120A (en) | 2002-06-25 |
Family
ID=17966162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0015120-3A BR0015120A (en) | 1999-10-28 | 2000-10-25 | Benzamidine derivative or a pharmaceutically acceptable salt thereof, pharmaceutical composition, and, use of a benzamidine derivative or a pharmaceutically acceptable salt thereof |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US6555556B1 (en) |
| EP (1) | EP1245564B1 (en) |
| KR (1) | KR100642953B1 (en) |
| CN (2) | CN1572882A (en) |
| AT (1) | ATE322479T1 (en) |
| AU (1) | AU776193B2 (en) |
| BR (1) | BR0015120A (en) |
| CA (1) | CA2389156C (en) |
| CY (1) | CY1106116T1 (en) |
| CZ (1) | CZ20021432A3 (en) |
| DE (1) | DE60027204T2 (en) |
| DK (1) | DK1245564T3 (en) |
| ES (1) | ES2261248T3 (en) |
| HK (1) | HK1047431B (en) |
| HU (1) | HUP0203161A3 (en) |
| IL (2) | IL149306A0 (en) |
| MX (1) | MXPA02004218A (en) |
| NO (1) | NO323147B1 (en) |
| NZ (1) | NZ518581A (en) |
| PL (1) | PL354619A1 (en) |
| PT (1) | PT1245564E (en) |
| RU (1) | RU2222529C2 (en) |
| TR (1) | TR200201654T2 (en) |
| TW (1) | TWI226886B (en) |
| WO (1) | WO2001030756A1 (en) |
| ZA (1) | ZA200203278B (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL354619A1 (en) * | 1999-10-28 | 2004-02-09 | Sankyo Company, Limited | Benzamidine derivatives |
| CN1610666A (en) * | 2001-04-05 | 2005-04-27 | 三共株式会社 | Benzamidine derivative |
| WO2002089803A1 (en) * | 2001-05-07 | 2002-11-14 | Sankyo Company, Limited | Composition for iontophoresis |
| EP1486485A4 (en) | 2002-03-15 | 2009-07-15 | Kissei Pharmaceutical | Novel crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative |
| CA2552766C (en) * | 2004-11-23 | 2010-08-17 | Dong Wha Pharmaceutical Ind. Co., Ltd. | N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine bis(methanesulfonate) |
| CN103159620A (en) * | 2013-03-28 | 2013-06-19 | 广西师范大学 | Preparation method of 2-hydroxyisophthalic acid |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA928276B (en) | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
| US5731324A (en) * | 1993-07-22 | 1998-03-24 | Eli Lilly And Company | Glycoprotein IIb/IIIa antagonists |
| ZA951617B (en) * | 1994-03-04 | 1997-02-27 | Lilly Co Eli | Antithrombotic agents. |
| NZ296210A (en) | 1994-12-02 | 1998-05-27 | Yamanouchi Pharma Co Ltd | Amidinonaphthyl derivatives to inhibit activated blood coagulation factor x |
| SI0906094T1 (en) * | 1996-01-02 | 2003-12-31 | Aventis Pharmaceuticals Inc. | Substituted n- (aminoiminomethyl or aminomethyl)phenyl)propyl amides |
| JP3565864B2 (en) * | 1996-09-12 | 2004-09-15 | シエーリング アクチエンゲゼルシヤフト | Benzamidine derivatives substituted by cyclic amino acids or cyclic hydroxy acid derivatives and their use as anti-pseudo-solids |
| TW542822B (en) | 1997-01-17 | 2003-07-21 | Ajinomoto Kk | Benzamidine derivatives |
| WO2000047553A2 (en) | 1999-02-11 | 2000-08-17 | Cor Therapeutics Inc. | ALKENYL AND ALKYNYL COMPOUNDS AS INHIBITORS OF FACTOR Xa |
| US6350761B1 (en) * | 1999-07-30 | 2002-02-26 | Berlex Laboratories, Inc. | Benzenamine derivatives as anti-coagulants |
| PL354619A1 (en) * | 1999-10-28 | 2004-02-09 | Sankyo Company, Limited | Benzamidine derivatives |
-
2000
- 2000-10-25 PL PL00354619A patent/PL354619A1/en unknown
- 2000-10-25 DE DE60027204T patent/DE60027204T2/en not_active Expired - Lifetime
- 2000-10-25 DK DK00970070T patent/DK1245564T3/en active
- 2000-10-25 MX MXPA02004218A patent/MXPA02004218A/en active IP Right Grant
- 2000-10-25 IL IL14930600A patent/IL149306A0/en active IP Right Grant
- 2000-10-25 NZ NZ518581A patent/NZ518581A/en unknown
- 2000-10-25 HU HU0203161A patent/HUP0203161A3/en unknown
- 2000-10-25 RU RU2002111343/04A patent/RU2222529C2/en not_active IP Right Cessation
- 2000-10-25 EP EP00970070A patent/EP1245564B1/en not_active Expired - Lifetime
- 2000-10-25 AU AU79574/00A patent/AU776193B2/en not_active Ceased
- 2000-10-25 CZ CZ20021432A patent/CZ20021432A3/en unknown
- 2000-10-25 ES ES00970070T patent/ES2261248T3/en not_active Expired - Lifetime
- 2000-10-25 AT AT00970070T patent/ATE322479T1/en not_active IP Right Cessation
- 2000-10-25 WO PCT/JP2000/007469 patent/WO2001030756A1/en active IP Right Grant
- 2000-10-25 PT PT00970070T patent/PT1245564E/en unknown
- 2000-10-25 TR TR2002/01654T patent/TR200201654T2/en unknown
- 2000-10-25 CN CNA2004100634713A patent/CN1572882A/en active Pending
- 2000-10-25 CN CNB008178003A patent/CN1293052C/en not_active Expired - Fee Related
- 2000-10-25 CA CA002389156A patent/CA2389156C/en not_active Expired - Fee Related
- 2000-10-25 KR KR1020027005382A patent/KR100642953B1/en not_active IP Right Cessation
- 2000-10-25 BR BR0015120-3A patent/BR0015120A/en not_active Application Discontinuation
- 2000-10-27 TW TW089122706A patent/TWI226886B/en not_active IP Right Cessation
-
2002
- 2002-04-23 IL IL149306A patent/IL149306A/en not_active IP Right Cessation
- 2002-04-24 ZA ZA200203278A patent/ZA200203278B/en unknown
- 2002-04-25 US US10/132,042 patent/US6555556B1/en not_active Expired - Fee Related
- 2002-04-26 NO NO20021990A patent/NO323147B1/en not_active IP Right Cessation
- 2002-11-06 US US10/288,838 patent/US20040010009A1/en not_active Abandoned
- 2002-12-05 HK HK02108844.9A patent/HK1047431B/en not_active IP Right Cessation
-
2003
- 2003-11-07 US US10/704,355 patent/US20040248981A1/en not_active Abandoned
-
2006
- 2006-07-04 CY CY20061100927T patent/CY1106116T1/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B11B | Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements |